Porfimer sodium
Identification
- Name
- Porfimer sodium
- Accession Number
- DB00707
- Description
The purified component of hematoporphyrin derivative, it consists of a mixture of oligomeric porphyrins. It is used in photodynamic therapy (hematoporphyrin photoradiation); to treat malignant lesions with visible light and experimentally as an antiviral agent. It is the first drug to be approved in the use of photodynamic therapy in the United States.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Synonyms
- Porfimer natrium
- Porfimer sodico
- Porfimer sodium
- Porfimère sodique
- Porfimerum natricum
Pharmacology
- Indication
Indicated in the treatment of esophageal cancer.
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- Pharmacodynamics
Porfimer is a photosensitizing agent used in the photodynamic therapy (PDT) of tumors. Porfimer is indicated for the palliation of patients with completely obstructing esophageal cancer, or of patients with partially obstructing esophageal cancer who cannot be satisfactorily treated with Nd:YAG laser therapy, reduction of obstruction and palliation of symptoms in patients with completely or partially obstructing endobronchial nonsmall cell lung cancer (NSCLC), and the treatment of microinvasive endobronchial NSCLC in patients for whom surgery and radiotherapy are not indicated. The cytotoxic and antitumor actions of porfimer are light and oxygen dependent. Tumor selectivity in treatment occurs through a combination of selective retention of porfimer and selective delivery of light.
- Mechanism of action
Cellular damage caused by porfimer is a consequence of the propagation of radical reactions. Radical initiation may occur after porfimer absorbs light to form a porphyrin excited state. Spin transfer from porfimer to molecular oxygen may then generate singlet oxygen. Subsequent radical reactions can form superoxide and hydroxyl radicals. Tumor death also occurs through ischemic necrosis secondary to vascular occlusion that appears to be partly mediated by thromboxane A2 release.
Target Actions Organism ULow-density lipoprotein receptor other/unknownHumans UHigh affinity immunoglobulin gamma Fc receptor I antagonistHumans - Absorption
- Not Available
- Volume of distribution
- 0.49 ± 0.28 L/kg [2 mg/kg dose of porfimer sodium to 4 male cancer patients]
- Protein binding
~90%
- Metabolism
- Not Available
- Route of elimination
- Not Available
- Half-life
10-452 hours
- Clearance
- Renal cl=199.7 +/- 56.9 mL/min [Healthy subjects receiving a single 300-mg oral dose]
- Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More- Toxicity
- Not Available
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Unlock Additional DataAminolevulinic acid Aminolevulinic acid may increase the photosensitizing activities of Porfimer sodium. Carprofen Carprofen may increase the photosensitizing activities of Porfimer sodium. Darbepoetin alfa The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Porfimer sodium. Erythropoietin The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Porfimer sodium. Hexaminolevulinate Hexaminolevulinate may increase the photosensitizing activities of Porfimer sodium. Methoxsalen Methoxsalen may increase the photosensitizing activities of Porfimer sodium. Methoxy polyethylene glycol-epoetin beta The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Porfimer sodium. Peginesatide The risk or severity of Thrombosis can be increased when Peginesatide is combined with Porfimer sodium. Riboflavin Riboflavin may increase the photosensitizing activities of Porfimer sodium. Temoporfin Temoporfin may increase the photosensitizing activities of Porfimer sodium. Additional Data Available- Extended DescriptionExtended DescriptionAvailable for Purchase
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - SeveritySeverityAvailable for Purchase
A severity rating for each drug interaction, from minor to major.
Learn more - Evidence LevelEvidence LevelAvailable for Purchase
A rating for the strength of the evidence supporting each drug interaction.
Learn more - ActionActionAvailable for Purchase
An effect category for each drug interaction. Know how this interaction affects the subject drug.
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- Food Interactions
- No interactions found.
Products
Purchasing individual compounds or compound libraries for your research?
Learn More- International/Other Brands
- PhotoBarr (Axcan) / Photofrin II
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataPhotofrin Powder, for solution 15 mg Intravenous Concordia Pharmaceuticals, Inc 1995-12-31 2014-11-21 Canada 
Photofrin Injection, powder, for solution 75 mg/31.8mL Intravenous Pinnacle Biologics, Inc. 1995-12-27 Not applicable US 
Photofrin Powder, for solution 75 mg Intravenous Concordia Pharmaceuticals, Inc 1995-12-31 2019-07-18 Canada Photofrin Injection, powder, for solution 2.5 mg/1mL Intravenous Axcan Scandipharm Inc. 2006-09-11 Not applicable US Additional Data Available- Application NumberApplication NumberAvailable for Purchase
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct CodeAvailable for Purchase
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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Categories
- ATC Codes
- L01XD01 — Porfimer sodium
- Drug Categories
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- Biological Factors
- Dermatologicals
- Hematoporphyrin Derivative
- Hematoporphyrins
- Heterocyclic Compounds, Fused-Ring
- Photoabsorption
- Photoactivated Radical Generator
- Photosensitizing Activity
- Photosensitizing Agents
- Photosensitizing agents used for phototherapy
- Pigments, Biological
- Porphyrins
- Radiation-Sensitizing Agents
- Sensitizers Used in Photodynamic/radiation Therapy
- Classification
- Not classified
Chemical Identifiers
- UNII
- Y3834SIK5F
- CAS number
- 87806-31-3
References
- General References
- Not Available
- External Links
- PubChem Substance
- 46508600
- ChemSpider
- 10482043
- 333848
- ChEBI
- 60652
- PharmGKB
- PA164752658
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Porfimer_sodium
- AHFS Codes
- 10:00.00 — Antineoplastic Agents
- FDA label
- Download (321 KB)
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Axcan pharma us inc
- Packagers
- Axcan Pharma Inc.
- Draxis Specialty Pharmaceuticals Inc.
- Dosage Forms
Form Route Strength Injection, powder, for solution Intravenous 2.5 mg/1mL Injection, powder, for solution Intravenous 75 mg/31.8mL Powder, for solution Intravenous 15 mg Powder, for solution Intravenous 75 mg - Prices
Unit description Cost Unit Photofrin 75 mg vial 3317.04USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region Unlock Additional DataUS5145863 No 1992-09-08 2009-12-15 US CA2094974 No 1996-10-22 2013-04-27 Canada Additional Data Available- Filed OnFiled OnAvailable for Purchase
The date on which a patent was filed with the relevant government.
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Properties
- State
- Solid
- Experimental Properties
Property Value Source logP 2.8 Not Available - Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Other/unknown
- General Function
- Virus receptor activity
- Specific Function
- Binds LDL, the major cholesterol-carrying lipoprotein of plasma, and transports it into cells by endocytosis. In order to be internalized, the receptor-ligand complexes must first cluster into clat...
- Gene Name
- LDLR
- Uniprot ID
- P01130
- Uniprot Name
- Low-density lipoprotein receptor
- Molecular Weight
- 95375.105 Da
References
- Korbelik M: Low density lipoprotein receptor pathway in the delivery of Photofrin: how much is it relevant for selective accumulation of the photosensitizer in tumors? J Photochem Photobiol B. 1992 Jan;12(1):107-9. [PubMed:1531856]
- Tsukagoshi S: [Porfimer sodium (Photofrin-II)]. Gan To Kagaku Ryoho. 1995 Aug;22(9):1271-8. [PubMed:7661580]
- Maziere JC, Mora L, Biade S, Maziere C, Santus R: [Potentiation of the photocytotoxic effect of photofrin II: synergistic action of verapamil and lovastatin]. Bull Acad Natl Med. 1994 Jun;178(6):1177-88; discussion 1188-9. [PubMed:7994588]
- Candide C, Morliere P, Maziere JC, Goldstein S, Santus R, Dubertret L, Reyftmann JP, Polonovski J: In vitro interaction of the photoactive anticancer porphyrin derivative photofrin II with low density lipoprotein, and its delivery to cultured human fibroblasts. FEBS Lett. 1986 Oct 20;207(1):133-8. [PubMed:2945739]
- Maziere JC, Morliere P, Biade S, Santus R: [Antitumor photochemotherapy: biochemical bases, therapeutic uses and perspectives]. C R Seances Soc Biol Fil. 1992;186(1-2):88-106. [PubMed:1450993]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Receptor signaling protein activity
- Specific Function
- High affinity receptor for the Fc region of immunoglobulins gamma. Functions in both innate and adaptive immune responses.
- Gene Name
- FCGR1A
- Uniprot ID
- P12314
- Uniprot Name
- High affinity immunoglobulin gamma Fc receptor I
- Molecular Weight
- 42631.525 Da
References
- Krutmann J, Athar M, Mendel DB, Khan IU, Guyre PM, Mukhtar H, Elmets CA: Inhibition of the high affinity Fc receptor (Fc gamma RI) on human monocytes by porphyrin photosensitization is highly specific and mediated by the generation of superoxide radicals. J Biol Chem. 1989 Jul 5;264(19):11407-13. [PubMed:2544592]
Drug created on June 13, 2005 07:24 / Updated on November 25, 2020 15:47
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